Synthesis and Characterization of a Gd-DOTA--Permeation Peptide for Magnetic Resonance Relaxation Enhancement of Intracellular Targets
Many MR contrast agents have been developed and proven effective for extracellular nontargeted applications, but exploitation of intracellular MR contrast agents has been elusive due to the permeability barrier of the plasma membrane. Peptide transduction domains can circumvent this permeability bar...
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| Format: | Article |
| Language: | English |
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SAGE Publishing
2003-10-01
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| Series: | Molecular Imaging |
| Online Access: | https://doi.org/10.1162/15353500200303106 |
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| _version_ | 1841563792089022464 |
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| author | Andrew M. Prantner Vijay Sharma Joel R. Garbow David Piwnica-Worms |
| author_facet | Andrew M. Prantner Vijay Sharma Joel R. Garbow David Piwnica-Worms |
| author_sort | Andrew M. Prantner |
| collection | DOAJ |
| description | Many MR contrast agents have been developed and proven effective for extracellular nontargeted applications, but exploitation of intracellular MR contrast agents has been elusive due to the permeability barrier of the plasma membrane. Peptide transduction domains can circumvent this permeability barrier and deliver cargo molecules to the cell interior. Based upon enhanced cellular uptake of permeation peptides with D -amino acid residues, an all-D Tat basic domain peptide was conjugated to DOTA and chelated to gadolinium. Gd-DOTA- D -Tat peptide in serum at room temperature showed a relaxivity of 7.94 ± 0.11 mM −1 sec −1 at 4.7 T. The peptide complex displayed no significant binding to serum proteins, was efficiently internalized by human Jurkat leukemia cells resulting in intracellular T1 relaxation enhancement, and in preliminary T1-weighted MRI experiments, significantly enhanced liver, kidney, and mesenteric signals. |
| format | Article |
| id | doaj-art-c614acfdd26244709bca19ac7c6bf0ab |
| institution | Kabale University |
| issn | 1536-0121 |
| language | English |
| publishDate | 2003-10-01 |
| publisher | SAGE Publishing |
| record_format | Article |
| series | Molecular Imaging |
| spelling | doaj-art-c614acfdd26244709bca19ac7c6bf0ab2025-01-02T23:37:28ZengSAGE PublishingMolecular Imaging1536-01212003-10-01210.1162/1535350020030310610.1162_15353500200303106Synthesis and Characterization of a Gd-DOTA--Permeation Peptide for Magnetic Resonance Relaxation Enhancement of Intracellular TargetsAndrew M. PrantnerVijay SharmaJoel R. GarbowDavid Piwnica-WormsMany MR contrast agents have been developed and proven effective for extracellular nontargeted applications, but exploitation of intracellular MR contrast agents has been elusive due to the permeability barrier of the plasma membrane. Peptide transduction domains can circumvent this permeability barrier and deliver cargo molecules to the cell interior. Based upon enhanced cellular uptake of permeation peptides with D -amino acid residues, an all-D Tat basic domain peptide was conjugated to DOTA and chelated to gadolinium. Gd-DOTA- D -Tat peptide in serum at room temperature showed a relaxivity of 7.94 ± 0.11 mM −1 sec −1 at 4.7 T. The peptide complex displayed no significant binding to serum proteins, was efficiently internalized by human Jurkat leukemia cells resulting in intracellular T1 relaxation enhancement, and in preliminary T1-weighted MRI experiments, significantly enhanced liver, kidney, and mesenteric signals.https://doi.org/10.1162/15353500200303106 |
| spellingShingle | Andrew M. Prantner Vijay Sharma Joel R. Garbow David Piwnica-Worms Synthesis and Characterization of a Gd-DOTA--Permeation Peptide for Magnetic Resonance Relaxation Enhancement of Intracellular Targets Molecular Imaging |
| title | Synthesis and Characterization of a Gd-DOTA--Permeation Peptide for Magnetic Resonance Relaxation Enhancement of Intracellular Targets |
| title_full | Synthesis and Characterization of a Gd-DOTA--Permeation Peptide for Magnetic Resonance Relaxation Enhancement of Intracellular Targets |
| title_fullStr | Synthesis and Characterization of a Gd-DOTA--Permeation Peptide for Magnetic Resonance Relaxation Enhancement of Intracellular Targets |
| title_full_unstemmed | Synthesis and Characterization of a Gd-DOTA--Permeation Peptide for Magnetic Resonance Relaxation Enhancement of Intracellular Targets |
| title_short | Synthesis and Characterization of a Gd-DOTA--Permeation Peptide for Magnetic Resonance Relaxation Enhancement of Intracellular Targets |
| title_sort | synthesis and characterization of a gd dota permeation peptide for magnetic resonance relaxation enhancement of intracellular targets |
| url | https://doi.org/10.1162/15353500200303106 |
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